TargetMol

Dacomitinib metabolite M2

Product Code:
 
TAR-T23950
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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Further Information

Bioactivity:
Dacomitinib metabolite M2 is also known as Dacomitinib cysteine conjugate. Dacomitinib inhibits both the wild-type (WT) EGFR and EGFR T790M.
CAS:
1262034-38-7
Molecular Weight:
591.1
Purity:
0.98
SMILES:
N(C=1C2=C(C=C(OC)C(NC(CC(CN3CCCCC3)SC[C@@H](C(O)=O)N)=O)=C2)N=CN1)C4=CC(Cl)=C(F)C=C4

References

Giri N, Masters JC, Plotka A, Liang Y, Boutros T, Pardo P, O'Connell J, Bello C. Investigation of the impact of hepatic impairment on the pharmacokinetics of dacomitinib. Invest New Drugs. 2015 Aug;33(4):931-41. doi: 10.1007/s10637-015-0256-0. Epub 2015 Jun 6. PubMed PMID: 26048096. Ramalingam SS, J?nne PA, Mok T, O'Byrne K, Boyer MJ, Von Pawel J, Pluzanski A, Shtivelband M, Docampo LI, Bennouna J, Zhang H, Liang JQ, Doherty JP, Taylor I, Mather CB, Goldberg Z, O'Connell J, Paz-Ares L. Dacomitinib versus erlotinib in patients with advanced-stage, previously treated non-small-cell lung cancer (ARCHER 1009): a randomised, double-blind, phase 3 trial. Lancet Oncol. 2014 Nov;15(12):1369-78. doi: 10.1016/S1470-2045(14)70452-8. Epub 2014 Oct 15. PubMed PMID: 25439691. Ellis PM, Shepherd FA, Millward M,et al; Australasian Lung Cancer Trials Group; NCI Naples Clinical Trials Unit. Dacomitinib compared with placebo in pretreated patients with advanced or metastatic non-small-cell lung cancer (NCIC CTG BR.26): a double-blind, randomised, phase 3 trial. Lancet Oncol. 2014 Nov;15(12):1379-88. doi: 10.1016/S1470-2045(14)70472-3. Epub 2014 Oct 15. PubMed PMID: 25439692. Ou SH, Soo RA. Dacomitinib in lung cancer: a "lost generation" EGFR tyrosine-kinase inhibitor from a bygone era? Drug Des Devel Ther. 2015 Oct 15;9:5641-53. doi: 10.2147/DDDT.S52787. eCollection 2015. Review. PubMed PMID: 26508839; PubMed Central PMCID: PMC4610796.